title: Synthesis of 4-aminoquinoline-pyrimidine hybrids as potent antimalarials and their mode of action studies.
abstract: One of the most viable options to tackle the growing resistance to the antimalarial drugs such as artemisinin is to resort to synthetic drugs. The multi-target strategy involving the use of hybrid drugs has shown promise. In line with this, new hybrids of quinoline with pyrimidine have been synthesized and evaluated for their antiplasmodial activity against both CQ(S) and CQ(R) strains of Plasmodium falciparum. These depicted activity in nanomolar range and were found to bind to heme as well as AT rich pUC18 DNA.
authors.affiliation: Department of Chemistry, UGC-Centre of Advance Study-1, Guru Nanak Dev University, Amritsar, Punjab 143005, India. kamaljit19in@yahoo.co.in
authors.forename: Kamaljit
authors.initials: K
authors.lastname: Singh
authors.forename: Hardeep
authors.initials: H
authors.lastname: Kaur
authors.forename: Kelly
authors.initials: K
authors.lastname: Chibale
authors.forename: Jan
authors.initials: J
authors.lastname: Balzarini
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D002460:Cell Line; D060326:Chemistry Techniques, Synthetic; D004247:DNA / Q000378:metabolism; D006418:Heme / Q000378:metabolism; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D000998:Antiviral Agents; D011743:Pyrimidines; D006418:Heme; D004247:DNA; C030986:pyrimidine
keywords: 4-Aminoquinolines; Antimalarials; Drug discovery; Heme binding; Hybrid molecules